PNU-159682

SKU: orb1307863

Description

PNU-159682 is a potent DNA topoisomerase II inhibitor derived from the anthracycline nemorubicin. This cytotoxic metabolite is utilized in cancer research to study its antitumor mechanisms in both in vitro and in vivo experimental models.

Research Area

Molecular Biology

Key Properties

• CAS Number: 202350-68-3
• MW: 641.62
• Purity: 99.08% (May vary between batches)
• Formula: C₃₂H₃₅NO₁₃
• SMILES: CO[C@H]1OCCN2[C@H]3C[C@H](O[C@H]4C[C@@](O)(Cc5c(O)c6C(=O)c7cccc(OC)c7C(=O)c6c(O)c45)C(=O)CO)O[C@@H](C)[C@H]3O[C@H]12
• Target: Topoisomerase,ADC Cytotoxin
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (5.14 mM);DMSO:96.7 mg/mL (150.71 mM)

Bioactivity

• Target IC50:
  CA IX:25 nM|Topo II unknotting activity:100 μM
• In Vivo:
  PNU-159682 (25 nmol/kg) shows an effective antitumor effect in mice bearing SKRC-52 xenografted tumors. PNU-159682 (15 μg/kg, i.v.) displays antitumor activity in mice bearing disseminated murine L1210 leukemia and in MX-1 human mammary carcinoma xenografts at 4 μg/kg.
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• In Vitro:
  PNU-159682 inhibits a panel of human tumor cell lines (IC70 values in the range of 0.07-0.58 nM). PNU-159682 is 2,360- to 790-fold and 6,420- to 2,100-fold more potent than MMDX and doxorubicin, respectively. PNU-159682 displays cytotoxic effect on CAIX-expressing SKRC-52 cells (IC50: 25 nM). PNU-159682 (10 μM)-DNA adducts contain one or two drug molecules bound to double-stranded DNA. PNU-159682 (100 μM) weakly inhibits topoisomerase II unknotting activity .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NMS249, NHL, non-Hodgkin's lymphoma, inhibit, Inhibitor, EDV nanocell, acute myeloid leukemia, ADC Payload, ADCs Toxin, ADCCytotoxin, ADC Cytotoxin, AML, Daunorubicins/Doxorubicins, Topoisomerase, topoisomerase I, PNU159682, PNU-159682, PNU 159682

Compound Identifiers

PubChem CID

9874188